Fluorescent ligands are versatile tools for the study of G protein-coupled receptors. Depending on the fluorophore, they can be used for a range of different applications, including fluorescence microscopy and bioluminescence or fluorescence resonance energy transfer (BRET or FRET) assays. Starting from phenylpiperazines and indanylamines, privileged scaffolds for dopamine D-like receptors, we developed dansyl-labeled fluorescent ligands that are well accommodated in the binding pockets of D and D receptors. These receptors are the target proteins for the therapy for several neurologic and psychiatric disorders, including Parkinson's disease and schizophrenia. The dansyl-labeled ligands exhibit binding affinities up to 0.44 nM and 0.29 nM at DR and DR, respectively. When the dansyl label was exchanged for sterically more demanding xanthene or cyanine dyes, fluorescent ligands 10a-c retained excellent binding properties and, as expected from their indanylamine pharmacophore, acted as agonists at DR. While the Cy3B-labeled ligand 10b was used to visualize DR and DR on the surface of living cells by total internal reflection microscopy, ligand 10a comprising a rhodamine label showed excellent properties in a NanoBRET binding assay at DR.
Download full-text PDF |
Source |
---|---|
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7736868 | PMC |
http://dx.doi.org/10.1038/s41598-020-78827-9 | DOI Listing |
Anal Chem
January 2025
Beijing National Laboratory for Molecular Sciences, Key Laboratory of Analytical Chemistry for Living Biosystems, Institute of Chemistry, Chinese Academy of Sciences, Beijing 100190, China.
Ligand binding to membrane proteins initiates numerous therapeutic processes. Surface plasmon resonance (SPR), a popular method for analyzing molecular interactions, has emerged as a promising tool for in situ determination of membrane protein binding kinetics owing to its label-free detection, high surface sensitivity, and resistance to intracellular interference. However, the excitation of SPR relies on noble metal films, typically gold, which are biologically incompatible and can cause fluorescence quenching.
View Article and Find Full Text PDFACS Appl Mater Interfaces
January 2025
Interdisciplinary Nanoscience Center, Aarhus University, Gustav Wieds Vej 14, 8000 Aarhus C, Denmark.
High-throughput measurement of cellular traction forces at the nanoscale remains a significant challenge in mechanobiology, limiting our understanding of how cells interact with their microenvironment. Here, we present a novel technique for fabricating protein nanopatterns in standard multiwell microplate formats (96/384-wells), enabling the high-throughput quantification of cellular forces using DNA tension gauge tethers (TGTs) amplified by CRISPR-Cas12a. Our method employs sparse colloidal lithography to create nanopatterned surfaces with feature sizes ranging from sub 100 to 800 nm on transparent, planar, and fully PEGylated substrates.
View Article and Find Full Text PDFJ Phys Chem Lett
January 2025
School of Biomedical Engineering, Shanghai Jiao Tong University, Shanghai 200240, P.R. China.
Gold nanoclusters (Au NCs) protected by molecular ligands represent a new class of second-generation near-infrared (NIR-II) luminescent materials that have been widely studied. However, the photoluminescence efficiencies of most NIR-II emitting Au NCs in aqueous solution are generally lower than 0.2%, and to fully exploit the advantages of AuNCs in the NIR-II region, improving their photoluminescence efficiency has become an urgent need.
View Article and Find Full Text PDFFront Immunol
January 2025
Department of Urology, National Cancer Center/National Clinical Research Center for Cancer/Cancer Hospital Shenzhen Hospital, Chinese Academy of Medical Sciences and Peking Union Medical College, Shenzhen, China.
Prostate-Specific Membrane Antigen (PSMA) is a highly expressed and structurally unique target specific to prostate cancer (PCa). Diagnostic and therapeutic approaches in nuclear medicine, coupling PSMA ligands with radionuclides, have shown significant clinical success. PSMA-PET/CT effectively identifies tumors and metastatic lymph nodes for imaging purposes, while -PSMA-617 (Pluvicto) has received FDA approval for treating metastatic castration-resistant PCa (mCRPC).
View Article and Find Full Text PDFJ Agric Food Chem
January 2025
College of Quality and Technical Supervision, Hebei University, Baoding 071002, China.
The extensive use of tetracyclines in livestock poses health risks due to their residues in animal-derived food; therefore, developing simple detection methods to replace complex traditional approaches is of paramount importance. Here, we developed a dual-ligand zinc-based metal-organic framework material, Zn-BTC-BDC-NH (denoted as ZTD), for the detection of tetracyclines. The intrinsic blue fluorescence of ZTD was quenched upon the introduction of tetracyclines due to electron transfer from -NH of ZTD to -CO- and -OH groups of tetracycline molecules; meanwhile, the new green fluorescence emission was generated through π-π stacking between aromatic rings and the formation of complexes between Zn and C-O/C═O groups.
View Article and Find Full Text PDFEnter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!